• Archives of Pharmacal Research
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• 제21권6호
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• pp.651-656
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• 1998

A sensitive high-performance liquid chromatographic (HPLC) method for the determination of aloesin in plasma was developed. After solid-phase extraction from plasma and derivatization of aloesin and compound AD-1, which was prepared from aloesin as a internal standard, with 9-anthroylnitrile in the presence of quinuclidine, the derivatives were separated on a Inertsil ODS-3 column using acetonitrile/methanol/water (3:1:6) as a mobile phase, and detected fluorimetrically at 460nm with excitation at 360nm. The detection limit of aloesin was 3.2ng/ml in plasma (S/N=3).

• 약학회지
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• 제46권3호
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• pp.168-173
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• 2002

The physicochemical properties of aloesin, which has been recently found to reduce renal toxicity induced by cis-platin, were studied including solubility, partition coefficient ( $P_{c}$ ), osmolality, and stability. The solubility of aloesin was about 500 mg/mι, and the $P_{c}$ value for n-octanol/water was 1.01 $\pm$ 0.03. The degradation of aloesin followed the pseudo-first-order kinetics and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be 2.0~3.0. Some metal ions increased the degradation rate in the rank order of M $n^{2+}$ ＞ F $e^{3+}$ ＞ C $u^{2+}$ ＞ F $e^{2+}$. On the other hand, other metal ions such as B $i^{3+}$, $Ba^{2+}$, Z $n^{2+}$, N $i^{2+}$, $Co^{2+}$ and $Mg^{2+}$ did not show the unfavorable effects. After autoclaving, aloesin contents remaining were 81.8~98.8% of initial concentrations depending on pH. The most stable pH was 3.98 in the autoclaving. Osmolality increased linearly as concentration increased.sed.creased.sed.

• Nutrition Research and Practice
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• 제3권1호
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• pp.9-14
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• 2009

Aloe products are one of the top selling health-functional foods in Korea, however the adequate level of intake to achieve desirable effects are not well understood. The objective of this study was to determine the intestinal uptake and metabolism of physiologically active aloe components using in vitro intestinal absorption model. The Caco-2 cell monolayer and the everted gut sac were incubated with $5-50{\mu}M$ of aloin, aloe-emodin, and aloesin. The basolateral appearance of test compounds and their glucuronosyl or sulfated forms were quantified using HPLC. The % absorption of aloin, aloe-emodin, and aloesin was ranged from 5.51% to 6.60%, 6.60% to 11.32%, and 7.61% to 13.64%, respectively. Up to 18.15%, 18.18%, and 38.86% of aloin, aloe-emodin, and aloesin, respectively, was absorbed as glucuronidated or sulfated form. These results suggest that a significant amount is transformed during absorption. The absorption rate of test compounds except aloesin was similar in two models; more aloesin was absorbed in the everted gut sac than in the Caco-2 monolayer. These results provide information to establish adequate intake level of aloe supplements to maintain effective plasma level.

• Archives of Pharmacal Research
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• 제22권3호
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• pp.232-236
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• 1999

In this study, we present evidence that cotreatment of aloesin and arbutin inhibits tyrosinase activity in a synergistic manner by acting through a different action mechanism. Aloesin or arbutin similarly inhibited enzyme activity of human- and mushroom-tyrosinases with an IC50 value of 0.1 or 0.04 mM, respectively. Lineweaver-Burk plots of the enzyme kinetics data showed that aloesin inhibited tyrosinase activity noncompetitively with a Ki value of 5.3 mM, whereas arbutin did it competitively (Maeda, 1996). We then examined whether cotreatment of these agents inhibits the tyrosinase activity in a synergistic manner. The results showed that 0.01 mM aloesin in the presence of 0.03 mM arbutin inhibited activity of mushroom by 80% of the control value and the reverse was also true. The inhibitory effects were calculated to be synergistic according to the B rgi method. Taken together, we suggest that aloesin along with arbutin inhibits in synergy melanin production by combined mechanisms of noncompetitive and competitive inhibitions of tyrosinase activity.

• 약학회지
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• 제40권2호
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• pp.177-182
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• 1996

The contents of aloesin in aloe preparations were determined by HPLC. Aloesin was extracted 3 times with ethanol for 30 minutes. The ethanol extract was concentrated and suspend ed in saturated NaCl aqueous solution and successively partitioned with dichloromethane, n-butanol. Prepared samples were analyzed by HPLC on a reverse column(Inertsil ODS-2). In assay, internal standard was a puerarin and regression of calibration curve was 0.998. Recoveries of aloesin added to aloe preparation were 98~123(%).

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.191.2-192
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• 2003

This study was conducted to examine the effect of subchronic oral administration of aloesin on changes in the body weight and blood biochemistry in rats. Aloesin were given orally at a rate of 100 mg/kg every 12 hours for 15 days. The rats in the control group received isotonic saline. Thebody weight and food consumption were measured every 12hrs immediately prior to each treatment throughout the study period. (omitted)

• 한국식품과학회지
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• 제30권1호
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• pp.192-198
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• 1998

제초제 paraquat의주된 독성 기전이 인체내 대사과정중 생성되는 superoxide anion radical $(O_{2-})$에 의한 것이라고 최근 보고된 바, 항산화작용을 갖는 taurine을 가지고 paraquat 독성 경감 효과 및 억제 기전에 관한 실험을 하게 되었으며 다음과 같은 결론을 얻게 되었다. 혈액생화학적인자 분석을 종합해 보면 paraquat의 독성 경감효과는 taurine, aloesin, ${\beta}-carotene$ 중 taurine이 가장 우수하였으며, aloesin도 효과가 있는 것으로 나타났다. In vivo에서 taurine은 혈액생화학적 검사에서 paraquat에 의해 유도된 간독성 지표인 sGPT. sGOT치, 신장독성 지표인 BUN, creatinine치 및 조직 손상의 지표인 ALP, MDA치를 정상으로 회복시켰다. 폐조직중의 MDA량, ALP 활성 및 collagen 량이 정상치로 회복이 되었다. 이로써 taurine은 paraquat의 폐독성 및 각 장기의 독성을 효과적으로 경감 시켜 준다는 사실을 확인할 수 있었다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2003년도 Annual Meeting of KSAP : International Symposium on Pharmaceutical and Biomedical Sciences on Obesity
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• pp.62-62
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• 2003

It is now convincing that free radical generation is involved in the pathophy siological mechanisms of ischemic stroke, particularly in ischemia-reperfusion injury. The present study, therefore, examined neuroprotective effect of aloesin isolated from Aloe vera, which was known to have antioxidative activity, in a rat model of transient focal cerebral ischemia. Transient focal cerebral ischemia was induced by occlusion of middle cerebral artery for 2 hr with a silicone-coated 4-0 nylon monofilament in male Sprague-Dawley rats under isoflurane anesthesia Aloesin (1, 3, 10, 30 and 50 mg/kg/injection) was administered intravenously 3 times at 0.5, 2 and 4 hr after onset of ischemia. Neurological score was measured 24 hr after onset of ischemia immediately before sacrifice. Seven serial coronal slices of the brain were stained with 2,3,5-triphenyltetrazolium chloride and infarct size was measured using a computerized image analyzer. Treatment with the close of 1 or 50 mg/kg did not significantly reduce infarct volume compared with the saline vehicle-treated control group. However, treatments with the closes of 3 and 10 mg/kg significantly reduced both infarct volume and edema by approximately 47% compared with the control group, producing remarkable behavioral recovery effect. Treatment with the close of 30 mg/kg also significantly reduced infarct volume to a lesser extent by approximately 33% compared with the control group, but produced similar degree of behavioral recovery effect. In addition, general pharmacological studies showed that aloesin was a quite safe compound. The results suggest that aloesin can serve as a lead chemical for the development of neuroprotective agents by providing neuroprotection against focal ischemic neuronal injury.

• 한국식품저장유통학회지
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• 제31권2호
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• pp.315-323
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• 2024

현재 항염증 활성에 대한 효능이 검증된 acemannan과 aloesin을 다양한 비율로 혼합하여 비율에 따른 항염증 효능을 확인하고자 본 연구를 진행하였다. 항염증 활성은 NO, PGE₂, TNF-α 및 IL-6 생성량 및 염증 관련 단백질인 iNOS, COX-2의 발현량에 대한 효능을 검증하였다. Acemannan과 aloesin 각각의 NO 생성 저해 활성 결과와 혼합 시료인 AA-1, AA-2, AA-3, AA-4, AA-5의 NO 생성 저해 활성 결과를 비교하였을 때, 혼합 시료가 더 우수한 NO 생성 저해 활성을 나타내는 것을 확인하였다. 이후 최적의 배합 비율을 찾기 위해 PGE₂, TNF-α 및 IL-6 생성량에 대해 측정하였다. 그 결과, 시료 5종 모두 최종농도인 100 ㎍/mL 농도에서 LPS 단독 처리군 대비 저해 효과가 나타났으며, 이 중 AA-2의 저해 효과가 가장 높은 것을 확인하여 western blot을 통한 염증 관련 단백질 발현량은 AA-2를 이용하여 실험을 진행하였다. 염증 관련 단백질인 iNOS 및 COX-2의 발현량을 측정 결과, AA-2는 농도 의존적으로 감소하였으며, 최종 농도인 100 ㎍/mL 농도에서 LPS 단독 처리군 대비 각각 25% 이상의 억제 효과가 나타나는 것을 확인하였다. 이러한 결과들을 토대로 acemannan과 aloesin을 다양한 비율로 배합하였을 때, 항염증 활성을 가진 것을 확인하였으며, 이 중 acemannan과 aloesin이 1:2의 비율로 혼합되었을 때 가장 높은 항염증 활성을 나타내었다. 결론적으로 acemannan과 aloesin을 혼합한 시료는 다양한 기능성 소재로써 활용이 가능하며, 이후 항염증 활성 실험들의 기초자료로도 활용이 가능한 것을 확인하였다.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.303.1-303.1
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• 2002

Recent studies have suggested that the cerebral ischemia induced the neuronal cell death by mediating multiple mechanisms with necrosis and/or apoptosis. The present study examined neuroprotective mechanism of aloesin against transient focal cerebral ischemia. Aloesin. main component of aloe possesses various biological activates such as wound healing. anti-gastric ulcer. and chemopreventive activity. Transient focal cerebral ischemia was induced by 120 min MCAO. (omitted)